Target Validation Information
TTD ID T99799
Target Name Cholinesterase (BCHE)
Type of Target
Successful
Drug Potency against Target Drug Info IC50 = 236 nM [12]
(-)-DEBROMOFLUSTRAMINE B Drug Info IC50 = 1370 nM [22]
(-)-Phenethylcymserine Drug Info IC50 = 6 nM
(-)-Phenserine Drug Info IC50 = 1560 nM
(-)-Tolserine Drug Info IC50 = 1950 nM
(1'H-Phenothiazin-1'-yl)(piperidin-1-yl)methanone Drug Info Ki = 1560 nM [34]
(10H-phenothiazin-10-yl)(m-tolyl)methanone Drug Info Ki = 1900 nM [16]
(10H-phenothiazin-10-yl)(o-tolyl)methanone Drug Info Ki = 3100 nM [16]
(10H-phenothiazin-10-yl)(p-tolyl)methanone Drug Info Ki = 2500 nM [16]
(10H-phenothiazin-10-yl)(phenyl)methanone Drug Info Ki = 5800 nM [16]
(24S)-ethylcholesta-7,9(11),22(E)-triene-3b-ol Drug Info Ki = 4600 nM [4]
(3-bromophenyl)(10H-phenothiazin-10-yl)methanone Drug Info Ki = 600 nM [16]
(4-bromophenyl)(10H-phenothiazin-10-yl)methanone Drug Info Ki = 1300 nM [16]
(4-nitrophenyl)(10H-phenothiazin-10-yl)methanone Drug Info Ki = 820 nM [16]
(RS)-tacrine(10)-hupyridone Drug Info IC50 = 81.5 nM [20]
1,10-bis(pyridinium)-decane dibromide Drug Info IC50 = 5000 nM [33]
1,11-bis(pyridinium)-undecane dibromide Drug Info IC50 = 7000 nM [33]
1,2-bis(2,3-fluorophenyl)ethane-1,2-dione Drug Info Ki = 1270 nM [15]
1,2-di(10H-phenothiazin-10-yl)ethane-1,2-dione Drug Info Ki = 220 nM [16]
1,2-Di(berberine-9-O-yl)ethane dibromide Drug Info IC50 = 1110 nM [36]
1,2-indanedione Drug Info Ki = 2630 nM [18]
1,2-NAPHTHOQUINONE Drug Info Ki = 2290 nM [18]
1,3-Di(berberine-9-O-yl)ethane dibromide Drug Info IC50 = 531 nM [36]
1,4-Di(berberine-9-O-yl)ethane dibromide Drug Info IC50 = 231 nM [36]
1,9-bis(pyridinium)-nonane dibromide Drug Info IC50 = 6000 nM [33]
1-(10H-phenothiazin-10-yl)-2-phenylbutan-1-one Drug Info Ki = 400 nM [16]
1-(10H-phenothiazin-10-yl)-2-phenylethanone Drug Info Ki = 610 nM [16]
1-(10H-phenothiazin-10-yl)-2-phenylpropan-1-one Drug Info Ki = 560 nM [16]
1-(10H-phenothiazin-10-yl)-3-phenylbutan-1-one Drug Info Ki = 1700 nM [16]
1-(10H-phenothiazin-10-yl)-3-phenylpropan-1-one Drug Info Ki = 6200 nM [16]
1-(10H-phenothiazin-10-yl)-4-phenylbutan-1-one Drug Info Ki = 220 nM [16]
1-(3,4-dichlorobenzyl)-1H-indole-2,3-dione Drug Info Ki = 12600 nM [14]
1-methyl-3-(phenylcarbamoyloxy)pyridinium bromide Drug Info IC50 = 550 nM
2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-imine Drug Info IC50 = 7200 nM [8]
2-biphenyl-4-yl-1-phenothiazin-10-yl-ethanone Drug Info Ki = 1700 nM [16]
2-methoxyphenyl 10H-phenothiazine-10-carboxylate Drug Info Ki = 340 nM [21]
2-Methyl-beta-carboline-2-ium iodide Drug Info IC50 = 540 nM [35]
2-Propyl-beta-carboline-2-ium iodide Drug Info IC50 = 2305 nM [35]
24-ethyl-cholest-7-ene-3,5,6-triol Drug Info Ki = 2500 nM [4]
24-ethylcholest-6-ene-3,5-diol Drug Info Ki = 4200 nM [4]
3,4,5,6-Tetrachloro-[1,2]benzoquinone Drug Info Ki = 3200 nM [3]
3-(2-Diethylamino-acetamino)-rutaecarpine Drug Info IC50 = 17620 nM [30]
3-(2-Diethylamino-propionamino)-rutaecarpine Drug Info IC50 = 2848 nM [30]
3-(2-N-Piperidyl-propionamino)-rutaecarpine Drug Info IC50 = 2112 nM [30]
3-(2-N-Pyrrolyl-acetamino)-rutaecarpine Drug Info IC50 = 696.1 nM [30]
3-(2-N-Pyrrolyl-propionamino)-rutaecarpine Drug Info IC50 = 844.5 nM [30]
3-(dimethylamino)phenyl phenylcarbamate Drug Info IC50 = 18000 nM
3-chlorophenyl 10H-phenothiazine-10-carboxylate Drug Info Ki = 570 nM [21]
3-isopr-sal-cyclosal-d4TMP Drug Info IC50 = 4700 nM [13]
3-methoxyphenyl 10H-phenothiazine-10-carboxylate Drug Info Ki = 710 nM [21]
3-phenyl-cyclosal-d4TMP Drug Info IC50 = 350 nM [13]
3-sal-cyclosal-d4TMP Drug Info IC50 = 2300 nM [13]
3-[10-(benzylmethylamino)decyloxy]xanthen-9-one Drug Info IC50 = 100 nM [10]
3-[11-(benzylmethylamino)undecyloxy]xanthen-9-one Drug Info IC50 = 120 nM [10]
3-[12-(benzylmethylamino)dodecyloxy]xanthen-9-one Drug Info IC50 = 150 nM [10]
3-[3-(benzylmethylamino)propoxy]xanthen-9-one Drug Info IC50 = 8330 nM [10]
3-[4-(benzylmethylamino)butoxy]xanthen-9-one Drug Info IC50 = 2650 nM [10]
3-[5-(benzylmethylamino)pentyloxy]xanthen-9-one Drug Info IC50 = 2490 nM [10]
3-[6-(benzylmethylamino)hexyloxy]xanthen-9-one Drug Info IC50 = 1430 nM [10]
3-[7-(benzylmethylamino)-heptyloxy]xanthen-9-one Drug Info IC50 = 800 nM [10]
3-[8-(benzylmethylamino)octyloxy]xanthen-9-one Drug Info IC50 = 80 nM [10]
3-[9-(benzylmethylamino)nonyloxy]xanthen-9-one Drug Info IC50 = 100 nM [10]
4-chlorophenyl 10H-phenothiazine-10-carboxylate Drug Info Ki = 10500 nM [21]
4-ISOPROPYLPHENSERINE Drug Info IC50 = 240 nM [32]
4-methoxyphenyl 10H-phenothiazine-10-carboxylate Drug Info Ki = 2260 nM [21]
4-[4-(benzyloxy)piperidino]butyl benzoate Drug Info IC50 = 1890 nM [17]
4-[4-(benzyloxy)piperidino]butyl-3-chlorobenzoate Drug Info IC50 = 1350 nM [17]
4-[4-(benzyloxy)piperidino]butyl-3-fluorobenzoate Drug Info IC50 = 1580 nM [17]
4-[4-(benzyloxy)piperidino]butyl-4-chlorobenzoate Drug Info IC50 = 3520 nM [17]
4-[4-(benzyloxy)piperidino]butyl-4-fluorobenzoate Drug Info IC50 = 560 nM [17]
4-[4-(benzyloxy)piperidino]butyl-4-nitrobenzoate Drug Info IC50 = 5230 nM [17]
5,6-dinitroacenaphthoquinone Drug Info Ki = 3100 nM [18]
5-methyl-cyclosal-d4TMP Drug Info IC50 = 4600 nM [13]
6-chlorotacrine hydrochloride Drug Info IC50 = 916 nM [26]
6-hydroxy-1,2,9-trimethyl-9H-beta-carbolin-2-ium Drug Info IC50 = 2700 nM [9]
6-hydroxy-1,2-dimethyl-9H-beta-carbolin-2-ium Drug Info IC50 = 1600 nM [9]
6-hydroxy-2-methyl-9H-beta-carbolin-2-ium Drug Info IC50 = 8700 nM [9]
6-methoxy-1,2-dimethyl-9H-beta-carbolin-2-ium Drug Info IC50 = 1200 nM [9]
6-methoxy-1,9-dimethyl-9H-pyrido[3,4-b]indole Drug Info IC50 = 17400 nM [9]
6-methoxy-2-methyl-9H-beta-carbolin-2-ium Drug Info IC50 = 17500 nM [9]
7-Oxo-7H-dibenzo[de,g]quinoline Drug Info IC50 = 4010 nM [25]
9-Ethyl-2-methyl-beta-carboline-2-ium iodide Drug Info IC50 = 2019 nM [35]
9-O-[2-(Phenylol-1-yloxy)ethyl]berberine bromide Drug Info IC50 = 3000 nM [28]
9-O-[2-(Phenylol-1-yloxy)hexyl]berberine bromide Drug Info IC50 = 4180 nM [28]
9-O-[3-(2-Pyridinoxyl)butyl]-berberine bromide Drug Info IC50 = 4160 nM [36]
9-O-[3-(4-Bromo-phenoxyl)butyl]-berberine bromide Drug Info IC50 = 5440 nM [36]
9-O-[3-(4-Nitro-phenoxyl)butyl]-berberine bromide Drug Info IC50 = 2050 nM [36]
9-O-[3-(Phenylamino)propyl]-berberine bromide Drug Info IC50 = 1760 nM [36]
9-O-[3-(Phenylol-1-yloxy)propyl]berberine bromide Drug Info IC50 = 2220 nM [28]
9-O-[4-(Phenylol-1-yloxy)butyl]berberine bromide Drug Info Ki = 1020 nM [28]
9-O-[5-(Phenylol-1-yloxy)pentyl]berberine bromide Drug Info IC50 = 2690 nM [28]
ACENAPHTHOQUINONE Drug Info Ki = 2970 nM [18]
Anthracen-10-yl(10H-phenothiazin-10-yl)methanone Drug Info Ki = 3.5 nM [16]
AS-1397 Drug Info IC50 = 3370 nM [11]
BENZOQUINONE Drug Info Ki = 2050 nM [3]
Bis-7-tacrine Drug Info IC50 = 10.5 nM [37]
Bis-cyclosal-d4TMP Drug Info IC50 = 14000 nM [13]
Butyl 10H-phenothiazine-10-carboxylate Drug Info Ki = 13400 nM [21]
CAPROCTAMINE Drug Info IC50 = 11600 nM [24]
CHF-2819 Drug Info IC50 = 1700 nM [2]
CHLORANIL Drug Info Ki = 268 nM [3]
Cyclopentyl 10H-phenothiazine-10-carboxylate Drug Info Ki = 3190 nM [21]
Cyclosal-d4TMP Drug Info IC50 = 770 nM [13]
DEMETHYLDEBROMOFLUSTRAMINE B Drug Info IC50 = 260 nM [22]
Eptastigmine Drug Info IC50 = 5 nM [6]
HALOXYSTEROL A Drug Info Ki = 4500 nM [4]
HALOXYSTEROL B Drug Info Ki = 2500 nM [4]
Haloxysterol C Drug Info Ki = 18000 nM [4]
Haloxysterol D Drug Info Ki = 2200 nM [4]
Huprine X Drug Info Ki = 120 nM [7]
Iso-OMPA Drug Info IC50 = 733 nM [23]
Isopropyl 10H-phenothiazine-10-carboxylate Drug Info Ki = 18100 nM [21]
Isosorbide-2-(benzylcarbamate)-5-benzoate Drug Info IC50 = 4.3 nM [23]
Isosorbide-2-(benzylcarbamate)-5-mononitrate Drug Info IC50 = 3.6 nM [23]
Isosorbide-2-(butylcarbamate)-5-benzoate Drug Info IC50 = 72 nM [23]
Isosorbide-2-(butylcarbamate)-5-mononitrate Drug Info IC50 = 894 nM [23]
Isosorbide-2-(cyclohexylcarbamate)-5-mononitrate Drug Info IC50 = 2500 nM [23]
Isosorbide-2-(ethylcarbamate)-5-mononitrate Drug Info IC50 = 3900 nM [23]
Isosorbide-2-(methylcarbamate)-5-benzoate Drug Info IC50 = 669 nM [23]
Isosorbide-2-(methylcarbamate)-5-mononitrate Drug Info IC50 = 5100 nM [23]
Isosorbide-2-(propylcarbamate)-5-mononitrate Drug Info IC50 = 639 nM [23]
Isosorbide-2-benzyl carbamate Drug Info IC50 = 3700 nM [29]
Isosorbide-2-benzylcarbamate-5-(o-toluate) Drug Info IC50 = 1.2 nM [29]
Isosorbide-2-benzylcarbamate-5-acetate Drug Info IC50 = 4100 nM [23]
Isosorbide-2-benzylcarbamate-5-cyclopentanoate Drug Info IC50 = 6 nM [23]
Isosorbide-2-benzylcarbamate-5-cyclopropanoate Drug Info IC50 = 334 nM [23]
Isosorbide-2-benzylcarbamate-5-isonicotinate Drug Info IC50 = 88 nM [23]
Isosorbide-2-benzylcarbamate-5-nicotinate Drug Info IC50 = 57 nM [23]
Isosorbide-2-benzylcarbamate-5-pentanoate Drug Info IC50 = 700 nM [23]
Isosorbide-2-benzylcarbamate-5-propionate Drug Info IC50 = 980 nM [23]
Isosorbide-2-benzylcarbamate-5-triflate Drug Info IC50 = 359 nM [23]
Isosorbide-di-(benzylcarbamate) Drug Info IC50 = 400 nM [31]
Isosorbide-di-(butylcarbamate) Drug Info IC50 = 1220 nM [31]
Isosorbide-di-(propylcarbamate) Drug Info IC50 = 10400 nM [31]
LAWSARITOL Drug Info Ki = 3700 nM [4]
LIPOCRINE Drug Info IC50 = 11 nM [27]
M-tolyl 10H-phenothiazine-10-carboxylate Drug Info Ki = 1690 nM [21]
MEMOQUIN Drug Info IC50 = 1440 nM [27]
MEPTAZINOL Drug Info IC50 = 15000 nM [19]
Methyl 10H-phenothiazine-10-carboxylate Drug Info Ki = 10200 nM [21]
Morpholino(1'H-phenothiazin-1'-yl)methanone Drug Info Ki = 7100 nM [34]
N,N'-(1',10'-decylene)-bis-(-)-nor-MEP Drug Info IC50 = 17 nM [19]
N,N'-(1',11'-undecydene)-bis-(-)-nor-MEP Drug Info IC50 = 74 nM [19]
N,N'-(1',12'-dodecydene)-bis-(-)-nor-MEP Drug Info IC50 = 100 nM [19]
N,N'-(1',2'-ethylene)-bis-(-)-nor-MEP Drug Info IC50 = 125 nM [19]
N,N'-(1',3'-propylene)-bis-(-)-nor-MEP Drug Info IC50 = 132 nM [19]
N,N'-(1',4'-butylene)-bis-(-)-nor-MEP Drug Info IC50 = 104 nM [19]
N,N'-(1',5'-pentylene)-bis-(-)-nor-MEP Drug Info IC50 = 192 nM [19]
N,N'-(1',6-hexylene)-bis-(-)-nor-MEP Drug Info IC50 = 119 nM [19]
N,N'-(1',7'-heptylene)-bis-(-)-nor-MEP Drug Info IC50 = 102 nM [19]
N,N'-(1',8'-octylene)-bis-(-)-nor-MEP Drug Info IC50 = 63 nM [19]
N,N'-(1',9'-nonylene)-bis-(-)-nor-MEP Drug Info IC50 = 10 nM [19]
N,N-Diethyl-1'H-phenothiazine-1'-carboxamide Drug Info Ki = 1050 nM [34]
N,N-Diisopropyl-1'H-phenothiazine-1'-carboxamide Drug Info Ki = 180 nM [34]
N,N-Dimethyl-1'H-phenothiazine-1'-carboxamide Drug Info Ki = 9200 nM [34]
N,N-Dipropyl-1'H-phenothiazine-1'-carboxamide Drug Info Ki = 430 nM [34]
N-(Adamant-1-yl)-1'H-phenothiazine-1'-carboxamide Drug Info Ki = 350 nM [34]
N-Benzyl-1'H-phenothiazine-1'-carboxamide Drug Info Ki = 4450 nM [34]
N-benzyl-2-thiomorpholinopyrimidin-4-amine Drug Info IC50 = 2300 nM [37]
N-Cyclobutyl-1'H-phenothiazine-1'-carboxamide Drug Info Ki = 10000 nM [34]
N-Cyclohexyl-1'H-phenothiazine-1'-carboxamide Drug Info Ki = 2810 nM [34]
N-Cyclopentyl-1'H-phenothiazine-1'-carboxamide Drug Info Ki = 2990 nM [34]
N-Isopropyl-1'H-phenothiazine-1'-carboxamide Drug Info Ki = 3410 nM [34]
N-Methyl-1'H-phenothiazine-1'-carboxamide Drug Info Ki = 18300 nM [34]
N-n-heptyl-7-methoxytacrine hydrochloride Drug Info IC50 = 40 nM [38]
N-n-hexyl-7-methoxytacrine hydrochloride Drug Info IC50 = 1000 nM [38]
N-n-nonyl-7-methoxytacrine hydrochloride Drug Info IC50 = 360 nM [38]
N-n-octyl-7-methoxytacrine hydrochloride Drug Info IC50 = 120 nM [38]
N-n-pentyl-7-methoxytacrine hydrochloride Drug Info IC50 = 16000 nM [38]
N-Neopentyl-1'H-phenothiazine-1'-carboxamide Drug Info Ki = 2660 nM [34]
N-o-Tolyl-1'H-phenothiazine-1'-carboxamide Drug Info Ki = 710 nM [34]
N-p-Tolyl-1'H-phenothiazine-1'-carboxamide Drug Info Ki = 12100 nM [34]
N-phenethyl-2-(pyrrolidin-1-yl)pyrimidin-4-amine Drug Info IC50 = 13800 nM [37]
N-Phenyl-1'H-phenothiazine-1'-carboxamide Drug Info Ki = 310 nM [34]
N-tert-Butyl-1'H-phenothiazine-1'-carboxamide Drug Info Ki = 10600 nM [34]
Naphthalen-1-yl 10H-phenothiazine-10-carboxylate Drug Info Ki = 36 nM [21]
Naphthalen-1-yl(10H-phenothiazin-10-yl)methanone Drug Info Ki = 88 nM [16]
Naphthalen-2-yl 10H-phenothiazine-10-carboxylate Drug Info Ki = 120 nM [21]
Naphthalen-2-yl(10H-phenothiazin-10-yl)methanone Drug Info Ki = 470 nM [16]
NOSTOCARBOLINE Drug Info IC50 = 13200 nM [5]
NSC-23180 Drug Info Ki = 1670 nM [18]
O-tolyl 10H-phenothiazine-10-carboxylate Drug Info Ki = 390 nM [21]
P-tolyl 10H-phenothiazine-10-carboxylate Drug Info Ki = 2850 nM [21]
Phenanthrene-9,10-dione Drug Info Ki = 190 nM [18]
Phenyl 10H-phenothiazine-10-carboxylate Drug Info Ki = 570 nM [21]
Tert-butyl 10H-phenothiazine-10-carboxylate Drug Info Ki = 4300 nM [21]
TOLSERINE Drug Info IC50 = 1950 nM [6]
VAGANINE D Drug Info IC50 = 10000 nM [1]
XANTHOSTIGMINE Drug Info IC50 = 48 nM [39]
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